公开(公告)号：US3900468A

公开(公告)日：1975-08-19

申请号：US22652672

申请日：1972-02-15

Applicant: ROUSSEL UCLAF

Inventor： MARTEL JACQUES ,  HEYMES RENE

IPC: C07D501/08 ,  A61K31/545 ,  C07C51/41 ,  C07D501/02 ,  C07D501/22 ,  C07D99/24

CPC classification number: C07C51/412 ,  Y02D70/12 ,  Y02D70/122 ,  C07C59/76

Abstract: Cis, trans and cis-trans mixtures of DL 7-R-amino-desacetoxycephalosporan compounds of the formula

wherein R is selected from the group consisting of hydrogen and trityl and R1 is selected from the group consisting of lower alkyl of 1 to 6 carbon atoms optionally substituted with at least one chlorine and aralkyl of 7 to 15 carbon atoms with the proviso when R is hydrogen, R1 is selected from the group consisting of tert.-butyl,benzyl and ethyl, processes for their preparation and novel intermediates produced therein.

公开(公告)号：US3707540A

公开(公告)日：1972-12-26

申请号：US3707540D

申请日：1966-12-07

Applicant: ROUSSEL UCLAF

Inventor： AMIARD GASTON ,  HEYMES RENE

IPC: C07D307/60 ,  C07D501/08 ,  C07D513/04 ,  G03C5/39 ,  C07D93/08 ,  C07D99/24

CPC classification number: C07D513/04 ,  C07D307/60 ,  G03C5/39

Abstract: LACTONES OF 2-(CARBONYL-AMINO-METHYL)-5-HYDROXYMETHYL-3,6-DIHYDRO-2H-1,3-THIAZINE-4 -CARBOXYLIC ACIDS USEFUL AS INTERMEDIATES FOR ANTIBIOTICS OF THE C-CEPHALOSPORINE FAMILY AND THEIR PREPARATION. THE INVENTION RELATES TO NOVEL DIHYDRO-1,3-THIAZINE COMPOUNDS OF THE FORMULA

2-(R-OOC-CH(-Y)-),7-(O=)-1,2,5,7-TETRAHYDRO-4H-FURO(3,4-D)

(3,1)THIAZINE

WHEREIN R IS SELECTED FROM THE GROUP CONSISTING OF ALKYL AND ARALKYL, Y IS SELECTED FROM THE GROUP CONSISTING OF -HN-AC, PHTHALIMIDO AND-NH-R'',R'' IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL AND ARALKYL AND AC IS THE ACYL RADICAL OF AN ORGANIC CARBOXYLIC ACID OF 1 TO 18 CARBON ATOMS AND TO A NOVEL PROCESS FOR THE PREPARATION OF THE SAID COMPOUNDS.

公开(公告)号：US3905965A

公开(公告)日：1975-09-16

申请号：US29777672

申请日：1972-10-16

Applicant: ROUSSEL UCLAF

Inventor： MARTEL JACQUES ,  HEYMES RENE

IPC: C07D513/04 ,  C07D279/04

CPC classification number: C07D501/46 ,  C07D513/04

Abstract: WHEREIN X'' IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL AND PHENYL LOWER ALKYL, R'' is selected from the group consisting of hydrogen, lower alkyl, phenyl, phenyl lower alkyl, lower alkyl phenyl, and Z'' is selected from the group consisting of amino and tritylamino. These compounds are useful as intermediates in the preparation of cephalosporin compounds.

A 1,3-thiazine compound having the formula

Abstract translation: 具有式WHEREIN X'的1,3-噻嗪化合物选自氢，低级烷基和苯基低级烷基，R'选自氢，低级烷基，苯基，苯基低级烷基，低级 烷基苯基，Z'选自氨基和三苯甲基氨基。

公开(公告)号：US3658802A

公开(公告)日：1972-04-25

申请号：US3658802D

申请日：1969-06-26

Applicant: ROUSSEL UCLAF

Inventor： HEYMES RENE ,  AMIARD GASTON ,  NOMINE GERARD

IPC: C07D501/46 ,  A61K31/545 ,  C07D20060101 ,  C07D501/04 ,  C07D501/38 ,  C07D501/60 ,  C07D99/24

CPC classification number: C07D501/38

Abstract: THIS INVENTION RELATES TO A CEPHALOSPORINE DERIVATIVE OF THE FORMULA

4-(R1-NH-),8-R2-1,3,4,4A,6,7-HEXAHYDRO-8H-AZETO(2,1-B)-

PYRROLO(3,4-D)(1,3)-THIAZINE

WHEREIN R1 REPRESENTS THE ACYL OF AN ORGANIC ACID AND R2 REPRESENTS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL, SUBSTITUTED ALKYL, ARYL AND SUBSTITUTED ARYL. THESE COMPOUNDS HAVE PARTICULARLY MARKED ANTIBIOTIC PROPERTIES, PARTICULARLY, A REMARKABLE ACTIVITY AGAINST STAPHYLOCOCCI.

公开(公告)号：US3642788A

公开(公告)日：1972-02-15

申请号：US3642788D

申请日：1967-03-13

Applicant: ROUSSEL UCLAF

Inventor： HEYMES RENE ,  AMIARD GASTON

IPC: C07D501/08 ,  C07D501/18 ,  C07D513/04 ,  C07D99/24

CPC classification number: C07D513/04

Abstract: THIS INVENTION RELATES TO A COMPOUND SELECTED FROM THE GROUP CONSISTING OF (1) A RACEMIC 6H,7H-CIS-7-AMINODESACETYLCEPHALOSPORANIC ACID DERIVATIVE OF THE FORMULA

2,3-(-COO-CH2-),7-(R-NH-)-2-CEPHEM

WHEREIN R IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND TRIPHENYLMETHYL, (2) IS OPTICALLY ACTIVE ANTIPODES AND (3) WHEN R IS HYDROGEN THEIR ACID ADDITION SALTS. THE INVENTION ALSO RELATES TO THE PROCESS OF PREPARING THESE COMPOUNDS. THESE COMPOUNDS ARE INTERMEDIATES USEFUL IN THE PREPARATION OF CEPHALOSPORIN ANTIBIOTICS AND THE 7-THIENYLACETYLAMINO DERIVATIVE POSSESSES AN ANTIBIOTIC ACTIVITY.